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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...
Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
GPCR Desensitization01:12

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...

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Related Experiment Video

Updated: May 21, 2026

BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
09:21

BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells

Published on: November 7, 2025

GPR35 as a Novel Therapeutic Target.

A E Mackenzie1, J E Lappin, D L Taylor

  • 1Molecular Pharmacology Group, Institute of Neuroscience and Psychology, College of Medical, Veterinary and Life Sciences, University of Glasgow Glasgow, UK.

Frontiers in Endocrinology
|June 2, 2012
PubMed
Summary
This summary is machine-generated.

G protein-coupled receptors (GPCRs) like GPR35 are targets for drug discovery. New ligands offer insights into GPR35

Keywords:
G-proteinsGPR35cardiovascular diseasediabetes

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Area of Science:

  • Pharmacology and drug discovery
  • Molecular and cellular biology
  • Receptor pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are crucial drug targets, yet many remain poorly understood.
  • GPR35, a GPCR discovered over a decade ago, has been an "orphan" receptor with undefined endogenous ligands.
  • Recent research has identified novel ligands for GPR35, sparking interest in its therapeutic potential.

Purpose of the Study:

  • To explore the characterization of the GPR35 receptor.
  • To investigate the role of GPR35 in various diseases.
  • To identify novel agonist and antagonist ligands for GPR35 to determine its physiological relevance.

Main Methods:

  • Review of recent publications on GPR35.
  • Analysis of identified endogenous and synthetic ligands.
  • Assessment of species-selective properties of ligands.
  • Evaluation of GPR35's role in disease models (in vitro and in vivo).

Main Results:

  • Novel potent ligands (endogenous and synthetic) for GPR35 have been identified.
  • Evidence suggests GPR35 involvement in diseases such as diabetes, hypertension, and asthma.
  • Identified ligands exhibit significant species-selective properties, posing drug development challenges.

Conclusions:

  • GPR35 is emerging as a promising therapeutic target for various diseases.
  • Further research is needed to fully elucidate GPR35's physiological roles and overcome drug development hurdles.
  • Identifying novel ligands is key to translating GPR35 research from in vitro and animal models to human applications.